Bisamine bisthiol radiolabel binding moieties

Abstract

This invention relates to bisamine bisthiol radiolabel binding moieties and synthetic methods therefor. Specifically, the invention provides radiolabel binding moieties that form an electrically neutral complex with technetium-99m.

What is claimed is: 
     
       1. A composition of matter comprising a bisamino bisthiol radiolabel binding moiety having a formula selected from the group consisting of: ##STR7## wherein each R is independently H, CH 3  or C 2  H 5  but if X=H, one R=Y; (pgp) N  =an amine protecting group or H;   each (pgp) S  is independently a thiol protecting group or H;   m, n and p are independently 2 or 3;   X=H or --A--COOH, but if X=H, one R=Y and (pgp) N  is not H;   Y=--A--COOH;   A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof, ##STR8## wherein each R is independently H, CH 3  or C 2  H 5  but if Z=H, one R=Y;   each (pgp) N  is an amine protecting group or H;   each (pgp) S  is independently a thiol protecting group or H;   m, n and p are independently 2 or 3;   Z=H or --A--CH(V)NH(pgp) 2   N , but if Z=H, one R=Y;   Y=--A--CH(V)NH(pgp) 2   N  ;   A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof;   V=H or COOH; and wherein if (pgp) N  and V are H, then (pgp) S  is not H and if (pgp) S  and V are H, then (pgp) N  is not H, and if V is H, (pgp) 1   N  is not H; and ##STR9## wherein each R is independently H, CH 3  or C 2  H 5  and one R=Y;     each (pgp) N  is an amine protecting group or H;   each (pgp) S  is independently a thiol protecting group or H;   m, n and p are independently 2 or 3;   Y=--A--CH(V)NH(pgp) 2   N  ;   A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof;   V=H or COOH; and wherein if (pgp) 2   N  and V are H, then (pgp) S  is not H and if (pgp) S  and V are H, then (pgp) 2   N  is not H, and at least one (pgp) 1   N  moiety is not H;   wherein the radiolabel-binding moiety is capable of forming an electrically neutral complex with a technetium-99m.